Application of compound 3,5,2',4'-tetrahydroxy chalcone in preparation of drug for preventing and treating hyperuricemia and gout

A technology of hydroxychalcone and hyperuricemia, which is applied in the application field of compound 3,5,2′,4′-tetrahydroxychalcone as a drug for the preparation and prevention of hyperuricemia and gout, and can solve the problem of blood uric acid Problems such as unsatisfactory activity

Inactive Publication Date: 2012-02-08
KUNMING MEDICAL UNIVERSITY +1
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  • Abstract
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  • Application Information

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Problems solved by technology

Among them, flavonoids have attracted much attention as a class of natural products. Quercetin, morin, myricetin, kaempferol, baicalein, puerarin, luteolin, daidzein, etc. have been found to have xanthine oxidase inhibitory activity , but the activity of reducing the blood uric acid level in hyperuricemia animals is not ideal. Therefore, it is meaningful to find or synthesize a new compound with higher uric acid-lowering potency in vivo

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  • Application of compound 3,5,2',4'-tetrahydroxy chalcone in preparation of drug for preventing and treating hyperuricemia and gout
  • Application of compound 3,5,2',4'-tetrahydroxy chalcone in preparation of drug for preventing and treating hyperuricemia and gout
  • Application of compound 3,5,2',4'-tetrahydroxy chalcone in preparation of drug for preventing and treating hyperuricemia and gout

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Embodiment Construction

[0019] (1) The compound of the present invention inhibits the medicinal efficacy of xanthine oxidase

[0020] Xanthine oxidase (EC 1.1.3.22) is a product of Sigma Company, prepared with sodium pyrophosphate buffer solution to an appropriate concentration for use. 3,5,2',4'-Tetrahydroxychalcone was prepared into a series of concentrations with sodium pyrophosphate buffer solution for use, and DMSO was used to aid dissolution. After incubating 3,5,2′,4′-tetrahydroxychalcone solutions with serial concentrations and xanthine oxidase at 25°C for 15 minutes, refer to the literature method [Zhu Shenyin, Zhou Yuanda, Liu Qingshan, Du Guanhua. Xanthine oxidase inhibition Establishment and application of drug high-throughput screening model. Chinese Journal of Pharmaceutical Sciences, 2007, 42 (3): 187-190] to measure the activity of xanthine oxidase, the results are as follows figure 2 It shows that 3,5,2',4'-tetrahydroxychalcone has a certain inhibitory effect on the activity of xan...

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Abstract

The invention discloses application of a compound 3,5,2',4'-tetrahydroxy chalcone in preparation of a drug for preventing and treating hyperuricemia and gout, relating to the application of drugs containing organic components. The compound obviously inhibits the activity of xanthine oxidase in vitro, wherein IC50 has the dosage of 22.5 mu mol / L and is a competitive inhibitor. In-vivo research shows that the compound has stronger gout resistant role, can obviously lower the uric acid level of serum of a rat with hyperuricemia induced by potassium oxonate or hypoxanthine by using 14.6 mu mol / kg(3.98mg / kg) dose, has less toxic and side effects, the maximum tolerance dose for intragastric administration of the rat being 5.0g / kg and obviously lower toxicity than gout resisting drugs used clinically at present, such as allopurinol, colchicin, benzbromarone, and the like, and can be used for preparing drugs and health care products for preventing and treating hyperuricemia and gout.

Description

technical field [0001] The invention belongs to medicines containing organic active ingredients. Background technique [0002] Gout is a group of metabolic diseases caused by the accumulation and precipitation of uric acid in the body due to excessive production of uric acid and / or decreased excretion of uric acid due to purine metabolic disorders. Uric acid is a product of purine metabolism in humans. Hyperuricemia is generally considered to be a sign of gout. According to statistics, about 5% to 12% of patients with hyperuricemia eventually develop gout. In Europe, North America, Japan and other regions and countries, the incidence of gout is relatively high, but with the improvement of people's living standards in our country, the extension of life span, the change of diet structure, and the increase of obese people, the incidence of gout has become higher than that of 15 years ago. It has increased by about 15 to 30 times, and it is no longer a rare disease of Chinese p...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/122A61P19/06A23L1/29A23L33/00
Inventor 李玲朱华结牛艳芬范华芳刘佳任洁
Owner KUNMING MEDICAL UNIVERSITY
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